1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Emedastine difumarate

Emedastine difumarate 

Cat. No.: HY-B2178
Handling Instructions

Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.

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Emedastine difumarate Chemical Structure

Emedastine difumarate Chemical Structure

CAS No. : 87233-62-3

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Description

Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].

IC50 & Target[1]

H1 Receptor

1.3 nM (Ki)

H2 Receptor

49067 nM (Ki)

H3 Receptor

12430 nM (Ki)

In Vitro

Emedastine difumarate inhibits histamine H2 receptor (Ki=49067 nM) and histamine H3 receptor (Ki=12430 nM)[1].
High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts[2].
Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration[2].

In Vivo

Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg[3].
Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B[3].
Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs[2].
Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM)[2].

Animal Model: Male ICR mice 5-6 weeks of age[3]
Dosage: 0.03, 0.1, 0.3 mg/kg
Administration: Orally; 30 min before pruritogen injection
Result: Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg.
Molecular Weight

534.56

Formula

C₂₅H₃₄N₄O₉

CAS No.

87233-62-3

SMILES

CN1CCN(C2=NC3=CC=CC=C3N2CCOCC)CCC1.O=C(O)/C=C/C(O)=O.O=C(O)/C=C/C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Emedastine difumarateHistamine ReceptororallybenzimidazoleantiallergicallergicrhinitisskindiseasesconjunctivitisInhibitorinhibitorinhibit

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